Imiquimod 50 mg/g Cream, 24 packets
🆔 Identity & classification
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🏷️ RxNorm drug class
This medicine belongs to the Antivirals class.
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🏭 Manufacturer & labeler
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🩺 Clinical
Imiquimod cream is used to treat certain types of actinic keratoses (flat, scaly growths on the skin caused by too much sun exposure), superficial basal cell carcinoma (a type of skin cancer), and warts on the skin of the genital and anal areas. Imiquimod is in a class of medications called immune response modifiers. It may work by increasing the activity of the body's immune system. Imiquimod cream does not cure warts, and new warts may appear during treatment. It is not known whether imiquimod cream prevents the spread of warts to other people.
Read the full MedlinePlus article ↗- Yes — and that's actually expected. Redness, flaking, and even some crusting or sores at the treatment site are a normal sign that the cream is doing its job. For actinic keratoses...
- How long does it take for imiquimod to work, and will the treated area look worse before it gets better?
- It's important to stick to the schedule your doctor prescribed — not more often. Using it more frequently than directed can make skin reactions much more severe without making trea...
- Can I use imiquimod every day to speed things up?
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Supplement & herbal interactions
Some supplements/herbs that may interact with Imiquimod — tap one for details:
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🧪 Inactive Ingredients / Excipients
Inactive ingredients, also called excipients, are components of the drug product other than the active ingredient. They may include fillers, dyes, coatings, preservatives, flavors, or other formulation ingredients.
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Benzyl alcohol is a clear liquid used as a preservative and solvent in medicines. It helps prevent bacterial and fungal growth and dissolves other ingredients to create uniform liquid formulations.
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Cetyl alcohol is a waxy, fatty substance derived from plant or animal sources. It acts as an emulsifier and thickener in medicines, helping blend oil and water components and giving products a smooth, creamy texture.
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Glycerin is a clear, thick liquid derived from plant oils or fats. It acts as a humectant to retain moisture, a sweetener, and a solvent in medications.
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Isostearic acid is a fatty acid derived from vegetable oils. It acts as an emulsifier and lubricant in medicines, helping blend ingredients together and reducing friction during tablet or capsule manufacturing.
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Methylparaben is a preservative derived from benzoic acid that prevents growth of bacteria, fungi, and mold in medicines. It extends the product's shelf life and maintains safety during storage.
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Petrolatum is a purified mineral oil-based jelly derived from petroleum. In medicines, it acts as an emollient, lubricant, and moisture barrier to soften skin, reduce friction, and help prevent water loss from formulations.
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A synthetic emulsifier derived from sorbitol and fatty acids. It helps mix oil and water-based ingredients together and improves the texture and stability of the medicine.
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Propylparaben is a chemical preservative used to prevent bacterial and fungal growth in medicines and personal care products. It helps extend shelf life and maintain product safety during storage.
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A waxy substance made from sorbitol and stearic acid. It acts as an emulsifier and stabilizer, helping keep oil and water mixed together and preventing separation in the medicine.
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Stearyl alcohol is a waxy, fatty substance derived from natural oils or made synthetically. It acts as an emulsifier and thickener in medicines, helping mix ingredients together and give the product the right texture.
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Water is a liquid solvent that dissolves and mixes ingredients together in liquid medicines, syrups, and injections. It helps distribute the active drug evenly throughout the product.
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Xanthan gum is a thickening and stabilizing ingredient made from fermented corn or other sugars. It's added to medicines to improve texture, prevent separation of liquids and solids, and help the product stay consistent.
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ingredient classCode="IACT" elements from the exact product block matched by this NDC. Label-section narrative from DailyMed / the openFDA label index is shown separately when available.Inactive ingredient FAQ
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💲 Pricing
A drug doesn't have one price. Each row is a different public payment system, and none is what you'd pay at the counter — that depends on your insurance. The ⓘ on each row explains what it measures.
| Price system | Per ea | Per package |
|---|---|---|
| Retail pharmacies payNADAC · weekly | $0.645 | $15.47 / 24 packets |
| Medicaid paysCMS SDUD · 12 mo | $1.23 | $29.40 / 24 packets |
| Medicare drug plans payPart D · Q2 2026 | $1.54 | $36.86 / 24 packets |
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🔁 Therapeutic equivalents
| Product | Labeler | Pack | NADAC/unit | TE | Status | Price vs. this |
|---|---|---|---|---|---|---|
| Imiquimod 50 mg/gthis 51672-4145-06 | Sun | 24 packets | $0.645 | AB | Availability likely | — |
| Imiquimod 50 mg/g 68462-0536-70 | Glenmark | 24 packets | $0.645 | AB | Availability likely | — |
| Imiquimod 12.5 mg/.25g 45802-0368-53 | Padagis | 12 packets | $12.145 | AB | Availability likely | +1784% |
| Imiquimod 12.5 mg/.25g 71335-2725-01 | Bryant | 24 packets | — | AB | FDA listed | — |
| Imiquimod 12.5 mg/.25g 71335-3000-01 | Bryant | 24 packets | — | AB | FDA listed | — |
| Imiquimod 12.5 mg/.25g 72162-2332-02 | Bryant | 24 packets | — | AB | FDA listed | — |
| Imiquimod 12.5 mg/.25g 72189-0084-24 | DIRECT | 25 g | — | AB | FDA listed | — |
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⏳ Availability & generic status
This product is an FDA-approved generic. Other versions of the same drug are listed under Therapeutic equivalents, least expensive first.
Where does this data come from?
🗺️ Medicaid utilization & spend
📊 Medicare Part D spend CMS · PART D · 2026 (Q1)
🔬 Reported adverse events (FAERS)
Top reported reactions
Reporter sex
Serious outcomes
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📦 Packaging — all sizes for this product
| Package NDC | Description | Marketing start | Status |
|---|---|---|---|
| 51672-4145-06 You're viewing this | 24 PACKET in 1 CARTON (51672-4145-6) / .25 g in 1 PACKET (51672-4145-8) | 2011-04-15 | Active |
📄 Full prescribing information FDA SPL
🚨 Boxed Warning ▾
Important: For use on the skin only (topical). Do not use Imiquimod Cream in or near your mouth, eyes, nose or vagina.
🎯 Indications and Usage ▾
1 INDICATIONS AND USAGE Imiquimod Cream USP, 5% is indicated for the topical treatment of: Clinically typical, nonhyperkeratotic, nonhypertrophic actinic keratoses (AK) on the face or scalp in immunocompetent adults ( 1.1 ). Biopsy-confirmed, primary superficial basal cell carcinoma (sBCC) in immunocompetent adults; maximum tumor diameter of 2.0 cm on trunk, neck, or extremities (excluding hands and feet), only when surgical methods are medically less appropriate and patient follow-up can be reasonably assured ( 1.2 ).
External genital and perianal warts/condyloma acuminata in patients 12 years old or older ( 1.3 ). Limitations of Use: Efficacy was not demonstrated for molluscum contagiosum in children aged 2-12 ( 1.4 , 8.4 )
1.1Actinic Keratosis Imiquimod Cream USP, 5% is indicated for the topical treatment of clinically typical, nonhyperkeratotic, nonhypertrophic actinic keratoses on the face or scalp in immunocompetent adults.
1.2Superficial Basal Cell Carcinoma Imiquimod Cream is indicated for the topical treatment of biopsy-confirmed, primary superficial basal cell carcinoma (sBCC) in immunocompetent adults, with a maximum tumor diameter of 2 cm, located on the trunk (excluding anogenital skin), neck, or extremities (excluding hands and feet), only when surgical methods are medically less appropriate and patient follow-up can be reasonably assured. The histological diagnosis of superficial basal cell carcinoma should be established prior to treatment, since safety and efficacy of imiquimod cream have not been established for other types of basal cell carcinomas, including nodular and morpheaform (fibrosing or sclerosing) types.
1.3External Genital Warts Imiquimod Cream USP, 5% is indicated for the treatment of external genital and perianal warts/condyloma acuminata in patients 12 years old or older.
1.4Limitations of Use Imiquimod Cream USP, 5% has been evaluated in children ages 2 to 12 years with molluscum contagiosum and these studies failed to demonstrate efficacy [see Use in Specific Populations (8.4) ].
1.5Unevaluated Populations The safety and efficacy of Imiquimod Cream USP, 5% in immunosuppressed patients have not been established. Imiquimod Cream should be used with caution in patients with pre-existing autoimmune conditions. The efficacy and safety of Imiquimod Cream have not been established for patients with Basal Cell Nevus Syndrome or Xeroderma Pigmentosum.
⏱️ Dosage and Administration ▾
2 DOSAGE AND ADMINISTRATION The application frequency for Imiquimod Cream is different for each indication. Imiquimod is not for oral, ophthalmic, or intravaginal use. Imiquimod Cream USP, 5% is not for oral, ophthalmic, or intravaginal use ( 2 ).
Actinic keratosis: 2 times per week for a full 16 weeks ( 2.1 ) Superficial basal cell carcinoma: 5 times per week for a full 6 weeks ( 2.2 ). External genital warts (EGW): 3 times per week until total clearance or a maximum of 16 weeks ( 2.3 ).
2.1Actinic Keratosis Imiquimod Cream should be applied 2 times per week for a full 16 weeks to a defined treatment area on the face or scalp (but not both concurrently). The treatment area is defined as one contiguous area of approximately 25 cm 2 (e.g., 5 cm × 5 cm) on the face (e.g., forehead or one cheek) or on the scalp. Examples of 2 times per week application schedules are Monday and Thursday, or Tuesday and Friday.
Imiquimod Cream should be applied to the entire treatment area and rubbed in until the cream is no longer visible. No more than one packet of Imiquimod Cream should be applied to the contiguous treatment area at each application. Imiquimod Cream should be applied prior to normal sleeping hours and left on the skin for approximately 8 hours, after which time the cream should be removed by washing the area with mild soap and water.
The prescriber should demonstrate the proper application technique to maximize the benefit of Imiquimod Cream therapy. It is recommended that patients wash their hands before and after applying Imiquimod Cream. Before applying the cream, the patient should wash the treatment area with mild soap and water and allow the area to dry thoroughly (at least 10 minutes).
Contact with the eyes, lips and nostrils should be avoided. Local skin reactions in the treatment area are common [see Adverse Reactions (6.1 , 6.5 )] . A rest period of several days may be taken if required by the patient's discomfort or severity of the local skin reaction.
However, the treatment period should not be extended beyond 16 weeks due to missed doses or rest periods. Response to treatment cannot be adequately assessed until resolution of local skin reactions. Lesions that do not respond to treatment should be carefully re-evaluated and management reconsidered.
Imiquimod Cream is packaged in single-use packets, with 24 packets supplied per box. Patients should be prescribed no more than 36 packets for the 16-week treatment period. Unused packets should be discarded.
Partially-used packets should be discarded and not reused.
2.2Superficial Basal Cell Carcinoma Imiquimod Cream should be applied 5 times per week for a full 6 weeks to a biopsy-confirmed superficial basal cell carcinoma. An example of a 5 times per week application schedule is to apply Imiquimod Cream, once per day, Monday through Friday. Imiquimod Cream should be applied prior to normal sleeping hours and left on the skin for approximately 8 hours, after which time the cream should be removed by washing the area with mild soap and water .
The prescriber should demonstrate the proper application technique to maximize the benefit of Imiquimod Cream therapy. It is recommended that patients wash their hands before and after applying Imiquimod Cream. The patient should wash the treatment area with mild soap and water before applying the cream, and allow the area to dry thoroughly.
The target tumor should have a maximum diameter of 2 cm and be located on the trunk (excluding anogenital skin), neck, or extremities (excluding hands and feet). The treatment area should include a 1 cm margin of skin around the tumor. Sufficient cream should be applied to cover the treatment area, including 1 centimeter of skin surrounding the tumor.
Imiquimod Cream should be rubbed into the treatment area until the cream is no longer visible. Table 1. Amount of Imiquimod Cream to Use for sBCC Target Tumor Diameter Size of Cream Droplet to be Used (diameter) Approximate Amount of Imiquimod to…
💊 Dosage Forms and Strengths ▾
3 DOSAGE FORMS AND STRENGTHS Imiquimod Cream USP, 5%, is supplied in single-use packets each of which contains 250 mg of the cream, equivalent to 12.5 mg of imiquimod. Imiquimod Cream is supplied in a box of 24 packets each. Imiquimod Cream USP, 5%, is supplied in single-use packets (24 per box), each of which contains 250 mg of the cream, equivalent to 12.5 mg of imiquimod ( 3 ).
⛔ Contraindications ▾
4 CONTRAINDICATIONS None. None ( 4 )
⚠️ Warnings and Cautions ▾
5 WARNINGS AND PRECAUTIONS Intense local inflammatory reactions can occur (e.g., skin weeping, erosion). Dosing interruption may be required ( 2 , 5.1 , 6 ). Severe local inflammatory reactions of the female external genitalia can lead to severe vulvar swelling.
Severe vulvar swelling can lead to urinary retention; dosing should be interrupted or discontinued. Flu-like systemic signs and symptoms including malaise, fever, nausea, myalgias and rigors may occur. Dosing interruption may be required ( 2 , 5.2 , 6 ).
Avoid exposure to sunlight and sunlamps. Wear sunscreen daily ( 5.3 ). Safety and efficacy have not been established for repeat courses of treatment to the same area for AK ( 5.4 ).
Imiquimod Cream is not recommended for treatment of BCC subtypes other than the superficial variant, i.e., sBCC( 5.5 ). Treatment of urethral, intra-vaginal, cervical, rectal or intra-anal viral disease is not recommended ( 5.6 ). Safety and efficacy in immunosuppressed patients have not been established ( 1.5 ).
5.1Local Inflammatory Reactions Intense local inflammatory reactions including skin weeping or erosion can occur after few applications of Imiquimod Cream and may require an interruption of dosing [see Dosage and Administration (2) and Adverse Reactions (6) ]. Imiquimod Cream has the potential to exacerbate inflammatory conditions of the skin, including chronic graft versus host disease. Severe local inflammatory reactions of the female external genitalia can lead to severe vulvar swelling.
Severe vulvar swelling can lead to urinary retention. Dosing should be interrupted or discontinued for severe vulvar swelling. Administration of Imiquimod Cream is not recommended until the skin is completely healed from any previous drug or surgical treatment.
5.2Systemic Reactions Flu-like signs and symptoms may accompany, or even precede, local inflammatory reactions and may include malaise, fever, nausea, myalgias and rigors. An interruption of dosing should be considered [see Adverse Reactions (6) ].
5.3Ultraviolet Light Exposure Exposure to sunlight (including sunlamps) should be avoided or minimized during use of Imiquimod Cream because of concern for heightened sunburn susceptibility. Patients should be warned to use protective clothing (e.g., a hat) when using Imiquimod Cream. Patients with sunburn should be advised not to use Imiquimod Cream until fully recovered.
Patients who may have considerable sun exposure, e.g., due to their occupation, and those patients with inherent sensitivity to sunlight should exercise caution when using Imiquimod Cream. Imiquimod Cream shortened the time to skin tumor formation in an animal photoco-carcinogenicity study [see Nonclinical Toxicology (13.1) ] . The enhancement of ultraviolet carcinogenicity is not necessarily dependent on phototoxic mechanisms.
Therefore, patients should minimize or avoid natural or artificial sunlight exposure.
5.4Unevaluated Uses: Actinic Keratosis Safety and efficacy have not been established for Imiquimod Cream in the treatment of actinic keratosis with repeated use, i.e., more than one treatment course, in the same area. The safety of Imiquimod Cream applied to areas of skin greater than 25 2 cm (e.g., 5 cm X 5 cm) for the treatment of actinic keratosis has not been established [see Clinical Pharmacology (12.3) ].
5.5Unevaluated Uses: Superficial Basal Cell Carcinoma The safety and efficacy of Imiquimod Cream have not been established for other types of basal cell carcinomas (BCC), including nodular and morpheaform (fibrosing or sclerosing) types. Imiquimod Cream is not recommended for treatment of BCC subtypes other than the superficial variant (i.e., sBCC) . Patients with sBCC treated with Imiquimod Cream should have regular followup of the treatment site [see Clinical Studies (14.2) ].
The safety and efficacy of treating sBCC lesions on the face, head and anogenital area have not been established.
5.6 Unevaluated Uses: External Genital Warts Imiquimod Cream has n…
🤒 Adverse Reactions ▾
6 ADVERSE REACTIONS Because clinical trials are conducted under widely varying conditions, adverse reaction rates observed in the clinical trials of a drug cannot be directly compared to rates in the clinical trials of another drug and may not reflect the rates observed in practice. Most common adverse reactions (incidence >28%) are application site reactions or local skin reactions: itching, burning, erythema, flaking/scaling/dryness, scabbing/crusting, edema, induration, excoriation, erosion, ulceration. Other reported reactions (≥1%) include fatigue, fever, and headache ( 6.1, 6.2 , 6.3 ).
To report SUSPECTED ADVERSE REACTIONS, contact Sun Pharmaceutical Industries, Inc., at 1-866-923-4914 or FDA at 1-800-FDA-1088 or www.fda.gov/medwatch.
6.1Clinical Trials Experience: Actinic Keratosis The data described below reflect exposure to Imiquimod Cream or vehicle in 436 subjects enrolled in two double-blind, vehicle-controlled studies. Subjects applied Imiquimod Cream or vehicle to a 25 cm 2 contiguous treatment area on the face or scalp 2 times per week for 16 weeks. Table 2: Selected Adverse Reactions Occurring in > 1% of Imiquimod-Treated Subjects and at a Greater Frequency than with Vehicle in the Combined Studies (Actinic Keratosis) Preferred Term Imiquimod Cream (n=215) Vehicle (n=221) Application Site Reaction 71 (33%) 32 (14%) Upper Resp Tract Infection 33 (15%) 27 (12%) Sinusitis 16 (7%) 14 (6%) Headache 11 (5%) 7 (3%) Carcinoma Squamous 8 (4%) 5 (2%) Diarrhea 6 (3%) 2 (1%) Eczema 4 (2%) 3 (1%) Back Pain 3 (1%) 2 (1%) Fatigue 3 (1%) 2 (1%) Fibrillation Atrial 3 (1%) 2 (1%) Infection Viral 3 (1%) 2 (1%) Dizziness 3 (1%) 1 (<1%) Vomiting 3 (1%) 1 (<1%) Urinary Tract Infection 3 (1%) 1 (<1%) Fever 3 (1%) 0 (0%) Rigors 3 (1%) 0 (0%) Alopecia 3 (1%) 0 (0%) Table 3: Application Site Reactions Reported by > 1% of Imiquimod-Treated Subjects and at a Greater Frequency than with Vehicle in the Combined Studies (Actinic Keratosis) Included Term Imiquimod Cream (n=215) Vehicle (n=221) Itching 44 (20%) 17 (8%) Burning 13 (6%) 4 (2%) Bleeding 7 (3%) 1 (<1%) Stinging 6 (3%) 2 (1%) Pain 6 (3%) 2 (1%) Induration 5 (2%) 3 (1%) Tenderness 4 (2%) 3 (1%) Irritation 4 (2%) 0 (0%) Local skin reactions were collected independently of the adverse reaction "application site reaction" in an effort to provide a better picture of the specific types of local reactions that might be seen.
The most frequently reported local skin reactions were erythema, flaking/scaling/dryness, and scabbing/crusting. The prevalence and severity of local skin reactions that occurred during controlled studies are shown in the following table. Table 4: Local Skin Reactions in the Treatment Area as Assessed by the Investigator (Actinic Keratosis) Imiquimod Cream (n=215) Vehicle (n=220) All Grades Mild, Moderate, or Severe Severe All Grades Severe Erythema 209 (97%) 38 (18%) 206 (93%) 5 (2%) Flaking/Scaling/Dryness 199 (93%) 16 (7%) 199 (91%) 7 (3%) Scabbing/Crusting 169 (79%) 18 (8%) 92 (42%) 4 (2%) Edema 106 (49%) 0 (0%) 22 (10%) 0 (0%) Erosion/Ulceration 103 (48%) 5 (2%) 20 (9%) 0 (0%) Weeping/Exudate 45 (22%) 0 (0%) 3 (1%) 0 (0%) Vesicles 19 (9%) 0 (0%) 2 (1%) 0 (0%) The adverse reactions that most frequently resulted in clinical intervention (e.g., rest periods, withdrawal from study) were local skin and application site reactions.
Overall, in the clinical studies, 2% (5/215) of subjects discontinued for local skin/application site reactions. Of the 215 subjects treated, 35 subjects (16%) on Imiquimod Cream and 3 of 220 subjects (1%) on vehicle cream had at least one rest period. Of these Imiquimod Cream subjects, 32 (91%) resumed therapy after a rest period.
In the AK studies, 22 of 678 (3.2%) of Imiquimod-treated subjects developed treatment site infections that required a rest period off Imiquimod Cream and were treated with antibiotics (19 with oral and 3 with topical). Of the 206 Imiquimod subjects with both baseline and 8-week post-treatment scarring assessments…
👥 Use in Specific Populations ▾
8 USE IN SPECIFIC POPULATIONS
8.1Pregnancy Pregnancy Category C: Note: The Maximum Recommended Human Dose (MRHD) was set at 2 packets per treatment of Imiquimod Cream (25 mg imiquimod) for the animal multiple of human exposure ratios presented in this label. If higher doses than 2 packets of Imiquimod Cream are used clinically, then the animal multiple of human exposure would be reduced for that dose. A non-proportional increase in systemic exposure with increased dose of Imiquimod Cream was noted in the clinical pharmacokinetic study conducted in actinic keratosis subjects [see Clinical Pharmacology (12.3) ] .
The AUC after topical application of 6 packets of Imiquimod Cream was 8 fold greater than the AUC after topical application of 2 packets of Imiquimod Cream in actinic keratosis subjects. Therefore, if a dose of 6 packets per treatment of Imiquimod Cream was topically administered to an individual, then the animal multiple of human exposure would be either 1/3 of the value provided in the label (based on body surface area comparisons) or 1/8 of the value provided in the label (based on AUC comparisons). The animal multiples of human exposure calculations were based on weekly dose comparisons for the carcinogenicity studies described in this label.
The animal multiples of human exposure calculations were based on daily dose comparisons for the reproductive toxicology studies described in this label. Systemic embryofetal development studies were conducted in rats and rabbits. Oral doses of 1, 5 and 20 mg/kg/day imiquimod were administered during the period of organogenesis (gestational days 6 – 15) to pregnant female rats.
In the presence of maternal toxicity, fetal effects noted at 20 mg/kg/day (577X MRHD based on AUC comparisons) included increased resorptions, decreased fetal body weights, delays in skeletal ossification, bent limb bones, and two fetuses in one litter (2 of 1567 fetuses) demonstrated exencephaly, protruding tongues and low-set ears. No treatment related effects on embryofetal toxicity or teratogenicity were noted at 5 mg/kg/day (98X MRHD based on AUC comparisons). Intravenous doses of 0.5, 1 and 2 mg/kg/day imiquimod were administered during the period of organogenesis (gestational days 6 – 18) to pregnant female rabbits.
No treatment related effects on embryofetal toxicity or teratogenicity were noted at 2 mg/kg/day (1.5X MRHD based on BSA comparisons), the highest dose evaluated in this study, or 1 mg/kg/day (407X MRHD based on AUC comparisons). A combined fertility and peri- and post-natal development study was conducted in rats. Oral doses of 1, 1.5, 3 and 6 mg/kg/day imiquimod were administered to male rats from 70 days prior to mating through the mating period and to female rats from 14 days prior to mating through parturition and lactation.
No effects on growth, fertility, reproduction or post-natal development were noted at doses up to 6 mg/kg/day (87X MRHD based on AUC comparisons), the highest dose evaluated in this study. In the absence of maternal toxicity, bent limb bones were noted in the F1 fetuses at a dose of 6 mg/kg/day (87X MRHD based on AUC comparisons). This fetal effect was also noted in the oral rat embryofetal development study conducted with imiquimod.
No treatment related effects on teratogenicity were noted at 3 mg/kg/day (41X MRHD based on AUC comparisons). There are no adequate and well-controlled studies in pregnant women. Imiquimod Cream should be used during pregnancy only if the potential benefit justifies the potential risk to the fetus.
8.3Nursing Mothers It is not known whether imiquimod is excreted in human milk following use of Imiquimod Cream. Because many drugs are excreted in human milk, caution should be exercised when Imiquimod Cream is administered to nursing women.
8.4Pediatric Use AK and sBCC are not conditions generally seen within the pediatric population. The safety and efficacy of Imiquimod Cream for AK or sBCC in patients less than 18 years of age ha…
🤰 Pregnancy ▾
8.1Pregnancy Pregnancy Category C: Note: The Maximum Recommended Human Dose (MRHD) was set at 2 packets per treatment of Imiquimod Cream (25 mg imiquimod) for the animal multiple of human exposure ratios presented in this label. If higher doses than 2 packets of Imiquimod Cream are used clinically, then the animal multiple of human exposure would be reduced for that dose. A non-proportional increase in systemic exposure with increased dose of Imiquimod Cream was noted in the clinical pharmacokinetic study conducted in actinic keratosis subjects [see Clinical Pharmacology (12.3) ] .
The AUC after topical application of 6 packets of Imiquimod Cream was 8 fold greater than the AUC after topical application of 2 packets of Imiquimod Cream in actinic keratosis subjects. Therefore, if a dose of 6 packets per treatment of Imiquimod Cream was topically administered to an individual, then the animal multiple of human exposure would be either 1/3 of the value provided in the label (based on body surface area comparisons) or 1/8 of the value provided in the label (based on AUC comparisons). The animal multiples of human exposure calculations were based on weekly dose comparisons for the carcinogenicity studies described in this label.
The animal multiples of human exposure calculations were based on daily dose comparisons for the reproductive toxicology studies described in this label. Systemic embryofetal development studies were conducted in rats and rabbits. Oral doses of 1, 5 and 20 mg/kg/day imiquimod were administered during the period of organogenesis (gestational days 6 – 15) to pregnant female rats.
In the presence of maternal toxicity, fetal effects noted at 20 mg/kg/day (577X MRHD based on AUC comparisons) included increased resorptions, decreased fetal body weights, delays in skeletal ossification, bent limb bones, and two fetuses in one litter (2 of 1567 fetuses) demonstrated exencephaly, protruding tongues and low-set ears. No treatment related effects on embryofetal toxicity or teratogenicity were noted at 5 mg/kg/day (98X MRHD based on AUC comparisons). Intravenous doses of 0.5, 1 and 2 mg/kg/day imiquimod were administered during the period of organogenesis (gestational days 6 – 18) to pregnant female rabbits.
No treatment related effects on embryofetal toxicity or teratogenicity were noted at 2 mg/kg/day (1.5X MRHD based on BSA comparisons), the highest dose evaluated in this study, or 1 mg/kg/day (407X MRHD based on AUC comparisons). A combined fertility and peri- and post-natal development study was conducted in rats. Oral doses of 1, 1.5, 3 and 6 mg/kg/day imiquimod were administered to male rats from 70 days prior to mating through the mating period and to female rats from 14 days prior to mating through parturition and lactation.
No effects on growth, fertility, reproduction or post-natal development were noted at doses up to 6 mg/kg/day (87X MRHD based on AUC comparisons), the highest dose evaluated in this study. In the absence of maternal toxicity, bent limb bones were noted in the F1 fetuses at a dose of 6 mg/kg/day (87X MRHD based on AUC comparisons). This fetal effect was also noted in the oral rat embryofetal development study conducted with imiquimod.
No treatment related effects on teratogenicity were noted at 3 mg/kg/day (41X MRHD based on AUC comparisons). There are no adequate and well-controlled studies in pregnant women. Imiquimod Cream should be used during pregnancy only if the potential benefit justifies the potential risk to the fetus.
🧒 Pediatric Use ▾
8.4Pediatric Use AK and sBCC are not conditions generally seen within the pediatric population. The safety and efficacy of Imiquimod Cream for AK or sBCC in patients less than 18 years of age have not been established. Safety and efficacy in patients with external genital/perianal warts below the age of 12 years have not been established.
Imiquimod Cream was evaluated in two randomized, vehicle-controlled, double-blind trials involving 702 pediatric subjects with molluscum contagiosum (MC) (470 exposed to Imiquimod; median age 5 years, range 2-12 years). Subjects applied Imiquimod Cream or vehicle 3 times weekly for up to 16 weeks. Complete clearance (no MC lesions) was assessed at Week 18.
In Study 1, the complete clearance rate was 24% (52/217) in the Imiquimod Cream group compared with 26% (28/106) in the vehicle group. In Study 2, the clearance rates were 24% (60/253) in the Imiquimod Cream group compared with 28% (35/126) in the vehicle group. These studies failed to demonstrate efficacy.
Similar to the studies conducted in adults, the most frequently reported adverse reaction from 2 studies in children with molluscum contagiosum was application site reaction. Adverse events which occurred more frequently in Imiquimod-treated subjects compared with vehicle-treated subjects generally resembled those seen in studies in indications approved for adults and also included otitis media (5% Imiquimod vs. 3% vehicle) and conjunctivitis (3% Imiquimod vs.
2% vehicle). Erythema was the most frequently reported local skin reaction. Severe local skin reactions reported by Imiquimod-treated subjects in the pediatric studies included erythema (28%), edema (8%), scabbing/crusting (5%), flaking/scaling (5%), erosion (2%) and weeping/exudate (2%).
Systemic absorption of imiquimod across the affected skin of 22 subjects aged 2 to 12 years with extensive MC involving at least 10% of the total body surface area was observed after single and multiple doses at a dosing frequency of 3 applications per week for 4 weeks. The investigator determined the dose applied, either 1, 2 or 3 packets per dose, based on the size of the treatment area and the subject's weight. The overall median peak serum drug concentrations at the end of week 4 was between 0.26 and 1.06 ng/mL except in a 2-year old female who was administered 2 packets of study drug per dose, had a C max of 9.66 ng/mL after multiple dosing.
Children aged 2 to 5 years received doses of 12.5 mg (one packet) or 25 mg (two packets) of imiquimod and had median multiple-dose peak serum drug levels of approximately 0.2 or 0.5 ng/mL, respectively. Children aged 6-12 years received doses of 12.5 mg, 25 mg, or 37.5 mg (three packets) and had median multiple dose serum drug levels of approximately 0.1, 0.15, or 0.3 ng/mL, respectively. Among the 20 subjects with evaluable laboratory assessments, the median WBC count decreased by 1.4*10 9 /L and the median absolute neutrophil count decreased by 1.42*10 9 /L.
🧓 Geriatric Use ▾
8.5Geriatric Use Of the 215 subjects treated with Imiquimod Cream in the AK clinical studies, 127 subjects (59%) were 65 years and older, while 60 subjects (28%) were 75 years and older. Of the 185 subjects treated with imiquimod Cream in the sBCC clinical studies, 65 subjects (35%) were 65 years and older, while 25 subjects (14%) were 75 years and older. No overall differences in safety or effectiveness were observed between these subjects and younger subjects.
No other clinical experience has identified differences in responses between the elderly and younger subjects, but greater sensitivity of some older individuals cannot be ruled out.
🆘 Overdosage ▾
10 OVERDOSAGE Topical overdosing of Imiquimod Cream could result in an increased incidence of severe local skin reactions and may increase the risk for systemic reactions. The most clinically serious adverse event reported following multiple oral imiquimod doses of >200 mg (equivalent to imiquimod content of >16 packets) was hypotension, which resolved following oral or intravenous fluid administration.
🧬 Clinical Pharmacology ▾
12 CLINICAL PHARMACOLOGY
12.1Mechanism of Action The mechanism of action of Imiquimod Cream in treating AK lesions is unknown.
12.2Pharmacodynamics Actinic Keratosis In a study of 18 subjects with AK comparing Imiquimod Cream to vehicle, increases from baseline in week 2 biomarker levels were reported for CD3, CD4, CD8, CD11c, and CD68 for Imiquimod Cream treated subjects; however, the clinical relevance of these findings is unknown. Superficial Basal Cell Carcinoma An open label study in six subjects with sBCC suggests that treatment with Imiquimod Cream may increase the infiltration of lymphocytes, dendritic cells, and macrophages into the tumor lesion; however, the clinical significance of these findings is unknown.
External Genital Warts Imiquimod has no direct antiviral activity in cell culture. A study in 22 subjects with genital/perianal warts comparing Imiquimod Cream and vehicle shows that Imiquimod Cream induces mRNA encoding cytokines including interferon- -α _ at the treatment site. In addition HPVL1 mRNA and HPV DNA are significantly decreased following treatment.
However, the clinical relevance of these findings is unknown.
12.3Pharmacokinetics Systemic absorption of imiquimod across the affected skin of 58 subjects with AK was observed with a dosing frequency of 3 applications per week for 16 weeks. Mean peak serum drug concentrations at the end of week 16 were approximately 0.1, 0.2, and 3.5 ng/mL for the applications to face (12.5 mg imiquimod, 1 single-use packet), scalp (25 mg, 2 packets) and hands/arms (75 mg, 6 packets), respectively. Table 10: Mean Serum Imiquimod Concentration in Adults Following Administration of the Last Topical Dose During Week 16 (Actinic Keratosis) Amount of Imiquimod Cream applied Mean peak serum imiquimod concentration [C max ] 12.5 mg (1 packet) 0.1 ng/mL 25 mg (2 packets) 0.2 ng/mL 75 mg (6 packets) 3.5 ng/mL The application surface area was not controlled when more than one packet was used.
Dose proportionality was not observed. However it appears that systemic exposure may be more dependent on surface area of application than amount of applied dose. The apparent half-life was approximately 10 times greater with topical dosing than the 2 hour apparent half-life seen following subcutaneous dosing, suggesting prolonged retention of drug in the skin.
Mean urinary recoveries of imiquimod and metabolites combined were 0.08 and 0.15% of the applied dose in the group using 75 mg (6 packets) for males and females, respectively following 3 applications per week for 16 weeks. Systemic absorption of imiquimod was observed across the affected skin of 12 subjects with genital/perianal warts, with an average dose of 4.6 mg. Mean peak drug concentration of approximately 0.4 ng/mL was seen during the study.
Mean urinary recoveries of imiquimod and metabolites combined over the whole course of treatment, expressed as percent of the estimated applied dose, were 0.11 and 2.41% in the males and females, respectively.
🧬 Mechanism of Action ▾
12.1Mechanism of Action The mechanism of action of Imiquimod Cream in treating AK lesions is unknown.
📦 How Supplied / Storage and Handling ▾
16 HOW SUPPLIED/STORAGE AND HANDLING Imiquimod Cream USP, 5%, is supplied in single-use packets which contain 250 mg of the cream: Box of 24 single-use packets – NDC 51672-4145-6 Discard unused packet. Store at 4° to 25°C (39° to 77°F) Avoid freezing. Keep out of reach of children.
📦 Storage and Handling ▾
Store at 4° to 25°C (39° to 77°F) Avoid freezing. Keep out of reach of children.
📋 Description ▾
11 DESCRIPTION Imiquimod Cream USP, 5% is an immune response modifier for topical administration. Each gram contains 50 mg of imiquimod in an off-white oil-in-water vanishing cream base consisting of benzyl alcohol, cetyl alcohol, glycerin, isostearic acid, methylparaben, polysorbate 60, propylparaben, purified water, sorbitan monostearate, stearyl alcohol, white petrolatum, and xanthan gum. Chemically, imiquimod is 1-(2-methylpropyl)-1 H -imidazo[4,5-c]quinolin-4-amine.
Imiquimod has a molecular formula of C 14 H 16 N 4 and a molecular weight of 240.3. Its structural formula is: Chemical Structure
💬 Information for Patients ▾
17 PATIENT COUNSELING INFORMATION See FDA-Approved Patient Labeling
17.1General Information: All Indications Imiquimod Cream should be used as directed by a physician [see Dosage and Administration (2) ] . Imiquimod Cream is for external use only. Contact with the eyes, lips and nostrils should be avoided. [see Indications and Usage (1) and Dosage and Administration (2) ] .
The treatment area should not be bandaged or otherwise occluded. Partially-used packets should be discarded and not reused. The prescriber should demonstrate the proper application technique to maximize the benefit of Imiquimod Cream therapy.
It is recommended that patients wash their hands before and after applying Imiquimod cream.
17.2Local Skin Reactions: All Indications Patients may experience local skin reactions during treatment with Imiquimod Cream (even with normal dosing). Potential local skin reactions include erythema, edema, vesicles, erosions/ulcerations, weeping/exudate, flaking/scaling/dryness, and scabbing/crusting. These reactions can range from mild to severe in intensity and may extend beyond the application site onto the surrounding skin.
Patients may also experience application site reactions such as itching and/or burning [see Adverse Reactions (6)] . Local skin reactions may be of such intensity that patients may require rest periods from treatment. Treatment with Imiquimod Cream can be resumed after the skin reaction has subsided, as determined by the physician.
Patients should contact their physician promptly if they experience any sign or symptom at the application site that restricts or prohibits their daily activity or makes continued application of the cream difficult. Because of local skin reactions, during treatment and until healed, the treatment area is likely to appear noticeably different from normal skin. Localized hypopigmentation and hyperpigmentation have been reported following use of Imiquimod Cream.
These skin color changes may be permanent in some patients.
17.3Systemic Reactions: All Indications Patients may experience flu-like systemic signs and symptoms during treatment with Imiquimod Cream (even with normal dosing). Systemic signs and symptoms may include malaise, fever, nausea, myalgias and rigors [see Adverse Reactions (6) ] . An interruption of dosing should be considered.
17.4Patients Being Treated for Actinic Keratosis (AK) Dosing is 2 times per week for a full 16 weeks, unless otherwise directed by the physician. However, the treatment period should not be extended beyond 16 weeks due to missed doses or rest periods [see Dosage and Administration (2.1) ] . It is recommended that the treatment area be washed with mild soap and water 8 hours following Imiquimod Cream application.
Most patients using Imiquimod Cream for the treatment of AK experience erythema, flaking/scaling/dryness and scabbing/crusting at the application site with normal dosing [see Adverse Reactions (6.1) ] . Use of sunscreen is encouraged, and patients should minimize or avoid exposure to natural or artificial sunlight (tanning beds or UVA/B treatment) while using Imiquimod Cream [see Warnings and Precautions (5.3) ] . Sub-clinical AK lesions may become apparent in the treatment area during treatment and may subsequently resolve [see Clinical Studies (14.1) ] .
17.5Patients Being Treated for Superficial Basal Cell Carcinoma (sBCC) Dosing is 5 times per week for a full 6 weeks, unless otherwise directed by the physician. However, the treatment period should not be extended beyond 6 weeks due to missed doses or rest periods [see Dosage and Administration (2.2) ] . It is recommended that the treatment area be washed with mild soap and water 8 hours following Imiquimod Cream application [see Dosage and Administration (2.2) ] .
Most patients using Imiquimod Cream for the treatment of sBCC experience erythema, edema, induration, erosion, scabbing/crusting and flaking/scaling at the application site with normal dosing [see Adverse Reactio…